Antimalarial in-vivo activity of bis(9-amino-6-chloro-2-methoxyacridines)

J Pharm Pharmacol. 2001 Jul;53(7):935-8. doi: 10.1211/0022357011776333.

Abstract

In the fight against malaria, chemotherapy using bisacridines may represent an alternative method to overcoming chloroquine-resistance. Eight bis(9-amino-6-chloro-2-methoxyacridines), in which acridine moieties were linked by polyamines substituted with a side chain, were tested for their in-vivo activity upon mice infected by Plasmodium berghei. Three of the compounds revealed antimalarial activity but no relationship could be deduced from a comparison of in-vitro and in-vivo activities. N-alkylation of the central amino group generated toxicity and, therefore, only compounds N-acylated in this position can be selected as leads.

Publication types

  • Research Support, Non-U.S. Gov't

MeSH terms

  • Aminoacridines / pharmacology*
  • Aminoacridines / therapeutic use
  • Animals
  • Antimalarials / chemistry
  • Antimalarials / pharmacology*
  • Antimalarials / therapeutic use
  • Chloroquine / pharmacology
  • Chloroquine / therapeutic use
  • Female
  • Malaria / drug therapy
  • Malaria / parasitology
  • Mice
  • Plasmodium berghei / drug effects*

Substances

  • Aminoacridines
  • Antimalarials
  • 9-amino-6-chloro-2-methoxyacridine
  • Chloroquine